New NEN Technology Geared to Boost High Throughput Screening Productivity for Drug Discovery; Fluorescence Polarization Technique Measures Changes in Molecular Rotation.

Business Editors and Health/Medical Writers

BOSTON--(BW HealthWire)--March 6, 2000

NEN Life Science Products has introduced a new, nonradioactive technology that will allow pharmaceutical R&D operations to dramatically improve their ability to rapidly and efficiently screen their increasingly vast libraries of potential drug candidates. The [FP]2(TM) family of homogeneous fluorescence polarization binding assays will, for the first time, provide HTS (high throughput screening) labs with a simple, robust, automation friendly and nonradioactive solution for screening GPCR (G protein-coupled receptor) targets.

Martin LeBlanc, General Manager of Advanced Bioconcept Co., an NEN subsidiary, said, "GPCR assays are one of the most important tools for drug discovery research today. Conducting these 'receptor binding assays' in a high throughput environment is challenging because the cumbersome, multiple steps required by conventional radioactive methods are difficult to automate, and results can be highly variable. These procedures also use large quantities of radioactive chemicals with heavily regulated and restrictive disposal procedures.

"The nonradioactive [FP]2 family of fluorescence polarization assays represents an impressive breakthrough, because they use a single-step, homogeneous 'mix and measure' protocol that has the potential to yield a step function productivity improvement for GPCR assays. Using advanced miniaturized 384- to 1536-well formats, a single automated system will have the potential to screen more than 100,000 assay points per day."

NEN is launching an initial selection of eight [FP]2 receptor binding assay kits. The kits are designed to provide a full range of solutions for GPCR HTS, from a successful first evaluation of the [FP]2 technology, to a fully validated assay for a primary screening project of a million compounds or more. All [FP]2 products feature Fluo-peptide ligands labeled with BODIPY(R)-TMR fluorescent dyes (Molecular Probes, Inc.). These red-shifted dyes are highly desirable for screening labs. Each kit is fully validated and includes an optimized buffer, detailed protocol and GPCR binding assay data. Other [FP]2 products and services include Custom Fluo-peptide Synthesis and Labeling Service and [FP]2 Assay Development Services.

The [FP]2 family reflects NEN's commitment to the development of new screening technologies, and is the result of extensive R&D efforts and invaluable customer collaborations. NEN's recent acquisition of Receptor Biology, Inc., a leading supplier of GPCR targets, is further evidence of NEN's continuing efforts in this important area of drug discovery.

NEN's [FP]2 high throughput screening assays rely on the principles of fluorescence polarization. When Fluo-peptides* (a unique and patented line of biologically active fluorescent reagents developed by Advanced Bioconcept) bind to a G protein-coupled receptor site, they increase the atomic weight of the molecule and slow its rotation. This, in turn, decreases the magnitude of polarization signal which can be detected with great precision by a high-speed reader. The signal is inversely proportional to the degree of binding (i.e., the smaller the signal, the higher percentage of binding.) More detailed information can be found at www.nen.com/fp2.

[FP]2 is the latest addition to NEN's growing line of drug discovery platforms and reagents including FlashPlate(R) scintillating microplates, radiolabeled ligands and substrates, cloned receptor membranes, and MICROMAX(TM) microarrays.

NEN Life Science Products is a leading provider of innovative labeling and detection products, services and technologies for life science research, drug discovery, and genomics applications. A privately held company with over 500 employees worldwide, NEN has facilities in Boston and Billerica, MA (USA), Brussels (Belgium), and Montreal, Quebec (Canada). For further information, contact: NEN Life Science Products, Inc., 549 Albany Street, Boston, MA, 02118, USA. Telephone: [phone] (U.S. Only) or [phone]. Fax: [phone]. In Europe, call [phone] or fax: [phone]. Website: nen.com.